Table 5.
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Fentanyl transdermal patch
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Buprenorphine transdermal patch
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| Absorption | Bioavailability, 92%; Plasma protein binding, 79%-87%; Cmax, 2.6 μg/L; Effective time, 12.7-16.6 h; Peak time 38.1 h; AUC, 117 μg/L; H (0-72 h) | Bioavailability, 50%; Plasma protein binding, 96%; Cmax, 305 pg/mL; Onset time 21 h; Peak time, about 60 h; AUC, 20228 pg/mL |
| Metabolism | Metabolized by CYP3A4 in the liver, and the metabolites are basically inactive | Metabolized by CYP3A4 in the liver |
| Elimination | The half-life of the transdermal patch is about 17 h (13-22 h) | The half-life of the transdermal patch is 25.3 h |
| Mechanism | μ opioid receptor agonist | μ opioid receptor partial agonist, δ opioid receptor agonist, weak κ opioid receptor antagonist, ORL-1 agonist |
| Indication | Moderate to severe chronic pain and intractable pain treated with opioid analgesics | Chronic pain beyond the control of nonopioid analgesics |
| Dosage form specification | 2.1-, 4.2-, 8.4- and 12.6-mg paste; Four specifications, lasting for 72 h | 5-, 10- and 20-mg paste. Each paste is used for 7 d |
| Adverse reactions, > 10% | Nausea, headache, constipation, dry mouth, drowsiness, fuzzy consciousness, powerlessness, sweating | Erythema, pruritus, nausea |
AUC: Area under the curve; ORL: Opioid receptor like; TDDS: Transdermal drug delivery system.